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3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
Semple G, Skinner PJ, Gharbaoui T, Shin YJ, Jung JK, Cherrier MC, Webb PJ, Tamura SY, Boatman PD, Sage CR, Schrader TO, Chen R, Colletti SL, Tata JR, Waters MG, Cheng K, Taggart AK, Cai TQ, Carballo-Jane E, Behan DP, Connolly DT, Richman JG. Semple G, et al. J Med Chem. 2008 Aug 28;51(16):5101-8. doi: 10.1021/jm800258p. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665582
Nicotinic acid receptor agonists differentially activate downstream effectors.
Richman JG, Kanemitsu-Parks M, Gaidarov I, Cameron JS, Griffin P, Zheng H, Guerra NC, Cham L, Maciejewski-Lenoir D, Behan DP, Boatman D, Chen R, Skinner P, Ornelas P, Waters MG, Wright SD, Semple G, Connolly DT. Richman JG, et al. Among authors: semple g. J Biol Chem. 2007 Jun 22;282(25):18028-18036. doi: 10.1074/jbc.M701866200. Epub 2007 Apr 23. J Biol Chem. 2007. PMID: 17452318 Free article.
Agonist lead identification for the high affinity niacin receptor GPR109a.
Gharbaoui T, Skinner PJ, Shin YJ, Averbuj C, Jung JK, Johnson BR, Duong T, Decaire M, Uy J, Cherrier MC, Webb PJ, Tamura SY, Zou N, Rodriguez N, Boatman PD, Sage CR, Lindstrom A, Xu J, Schrader TO, Smith BM, Chen R, Richman JG, Connolly DT, Colletti SL, Tata JR, Semple G. Gharbaoui T, et al. Among authors: semple g. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4914-9. doi: 10.1016/j.bmcl.2007.06.028. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17588745
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.
Skinner PJ, Cherrier MC, Webb PJ, Shin YJ, Gharbaoui T, Lindstrom A, Hong V, Tamura SY, Dang HT, Pride CC, Chen R, Richman JG, Connolly DT, Semple G. Skinner PJ, et al. Among authors: semple g. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5620-3. doi: 10.1016/j.bmcl.2007.07.101. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17804224
Nicotinic acid receptor agonists.
Boatman PD, Richman JG, Semple G. Boatman PD, et al. Among authors: semple g. J Med Chem. 2008 Dec 25;51(24):7653-62. doi: 10.1021/jm800896z. J Med Chem. 2008. PMID: 18983141 Review. No abstract available.
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG. Boatman PD, et al. Among authors: semple g. Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062. Epub 2010 Mar 20. Bioorg Med Chem Lett. 2010. PMID: 20363624
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